UA108863C2 - Бензоксепиновые ингибиторы pi3 и их применение - Google Patents

Бензоксепиновые ингибиторы pi3 и их применение

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Publication number
UA108863C2
UA108863C2 UAA201204809A UAA201204809A UA108863C2 UA 108863 C2 UA108863 C2 UA 108863C2 UA A201204809 A UAA201204809 A UA A201204809A UA A201204809 A UAA201204809 A UA A201204809A UA 108863 C2 UA108863 C2 UA 108863C2
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Ukraine
Prior art keywords
formula
compounds
lipid kinases
disorders
inhibitors
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UAA201204809A
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English (en)
Ukrainian (uk)
Inventor
Ніколь Блак'єр
Стівен До
Данетт Дадлі
Адріан Дж. Фоулкс
Річард А. Голдсміт
Роберт Хілд
Тім Хеффрон
Александр Колесніков
Чуді Ндубаку
Алан Дж. Оліверо
Стівен Прайс
Стівен Стейбен
БіньЦін Вей
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Ф. Хоффманн-Ля Рош Аг
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Application filed by Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of UA108863C2 publication Critical patent/UA108863C2/ru

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Abstract

В заявке описаны бензоксепины формулы I, включая стереоизомеры, геометрические изомеры, таутомеры, сольваты, метаболиты и фармацевтически приемлемые соли указанных соединений, где Z1 означает CR1 или N, Z2 означает CR2 или N, Z3 означает CR3 или N, Z4 означает CR4 или N, и где (1) X1 означает N, а X2 означает S (2) X1 означает S, а X2 означает N, (3) X1 означает CR7, a X2 означает S (4) X1 означает S, а X2 означает CR7, (5) X1 означает NR8, а X2 означает N (6) X1 означает N, а X2 означает NR8 (7) X1 означает CR7, а X2 означает О, (8) X1 означает О, а X2 означает CR7, (9 ) X1 означает CR7, a X2 означает C(R7)2, (10) X1 означает C(R7)2, а X2 означает CR7, (11) X1 означает N, а X2 означает О, или (12) X1 означает О, а X2 означает N, которые можно использовать для ингибирования липидкиназ, включая р110α а другие изоформы PI3K, и для лечения опосредованных липидкиназамы нарушений, таких как рак. В заявке описаны способы применения соединений формулы I для диагностики, профилактики или лечения in vitro, in situ и in vivo указанных нарушений или сопутствующих патологических состояний в клетках млекопитающих.
UAA201204809A 2009-09-28 2010-09-27 Бензоксепиновые ингибиторы pi3 и их применение UA108863C2 (ru)

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US24638609P 2009-09-28 2009-09-28
PCT/EP2010/064222 WO2011036284A1 (en) 2009-09-28 2010-09-27 Benzoxepin pi3k inhibitor compounds and methods of use

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Publication number Priority date Publication date Assignee Title
SI2483278T1 (sl) * 2009-09-28 2014-03-31 F. Hoffmann-La Roche Ag Inhibitorske spojine benzoksazepina pi3k in njihova uporaba pri zdravljenju raka
UA108863C2 (ru) * 2009-09-28 2015-06-25 Ф. Хоффманн-Ля Рош Аг Бензоксепиновые ингибиторы pi3 и их применение
RU2013143747A (ru) 2011-03-21 2015-04-27 Ф. Хоффманн-Ля Рош Аг Соединения бензоксазепина, селективные в отношении pi3k p110 дельта и способы их применения
WO2013030750A1 (en) 2011-09-01 2013-03-07 Lupin Limited Antiviral compounds
CN104284899A (zh) 2012-02-17 2015-01-14 弗·哈夫曼-拉罗切有限公司 三环化合物和其应用方法
EP2852661A1 (en) 2012-05-23 2015-04-01 F. Hoffmann-La Roche AG Compositions and methods of obtaining and using endoderm and hepatocyte cells
WO2013182668A1 (en) 2012-06-08 2013-12-12 F. Hoffmann-La Roche Ag Mutant selectivity and combinations of a phosphoinositide 3 kinase inhibitor compound and chemotherapeutic agents for the treatment of cancer
US9328106B2 (en) 2012-09-26 2016-05-03 Genentech, Inc. Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
ES2861180T3 (es) 2013-03-13 2021-10-05 Forma Therapeutics Inc Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etan-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer
KR101871133B1 (ko) 2013-03-13 2018-06-25 에프. 호프만-라 로슈 아게 벤즈옥사제핀 화합물의 제조 방법
CN103274963B (zh) * 2013-06-28 2015-12-23 江苏倍达医药科技有限公司 一种合成1，1，1-三氟异丙基肼盐酸盐的方法
AU2015240465B2 (en) 2014-04-04 2020-02-27 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
NO2714752T3 (ru) * 2014-05-08 2018-04-21
IL280856B (en) 2015-02-02 2022-09-01 Forma Therapeutics Inc 3-Alkyl-4-amino-[0,5,4] bicyclic hydroxamic acids as hdac inhibitors
TW201636329A (zh) 2015-02-02 2016-10-16 佛瑪治療公司 作為ｈｄａｃ抑制劑之雙環［４，６，０］異羥肟酸
RU2571094C1 (ru) * 2015-02-11 2015-12-20 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Омский государственный университет им. Ф.М. Достоевского" СПОСОБ ПОЛУЧЕНИЯ 4-АЛКОКСИ-4Н-ТИЕНО[3,2-с]ХРОМЕН-2-КАРБАЛЬДЕГИДОВ, ОБЛАДАЮЩИХ ПРОТИВОЯЗВЕННОЙ АКТИВНОСТЬЮ
EP3828269B1 (en) 2015-03-06 2023-05-03 Korea Advanced Institute Of Science And Technology Composition for prevention or treatment of intractable epilepsy comprising mtor inhibitor
EP3317283B1 (en) 2015-07-02 2019-04-03 H. Hoffnabb-La Roche Ag Benzoxazepin oxazolidinone compounds and methods of use
RS59740B1 (sr) * 2015-07-02 2020-02-28 Hoffmann La Roche Benzoksazepin oksazolidinonska jedinjenja i postupci upotrebe
CN112409378A (zh) 2015-09-08 2021-02-26 豪夫迈·罗氏有限公司 三环pi3k抑制剂化合物及其使用方法
AU2016319638B2 (en) * 2015-09-09 2021-02-11 Jubilant Biosys Limited Tricyclic fused pyridin-2-one derivatives and their use as BRD4 inhibitors
US10241701B2 (en) * 2015-09-16 2019-03-26 Samsung Electronics Co., Ltd. Solid state memory system with power management mechanism and method of operation thereof
GB201516504D0 (en) 2015-09-17 2015-11-04 Astrazeneca Ab Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer
EP3472131B1 (en) 2016-06-17 2020-02-19 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors
CN106317050B (zh) * 2016-08-24 2018-11-23 烟台大学 一种苯基噻唑衍生物及其制备方法与应用
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
CN113382633A (zh) 2018-10-29 2021-09-10 福马治疗股份有限公司 (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
GB8504702D0 (en) 1985-02-23 1985-03-27 Zyma Sa Tricyclic compounds
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
FR2677356B1 (fr) * 1991-06-05 1995-03-17 Sanofi Sa Derives heterocycliques d'acylamino-2 thiazoles-5 substitues, leur preparation et compositions pharmaceutiques en contenant.
US6274327B1 (en) 1992-04-13 2001-08-14 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
US5846824A (en) 1994-02-07 1998-12-08 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
DK0638071T3 (da) 1992-12-28 1997-10-27 Eisai Co Ltd Heterocykliske carboxylsyrederivater, der bindes til retenoidreceptorer (RAR)
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH08175990A (ja) 1994-12-19 1996-07-09 Mitsubishi Chem Corp Ｐｉ３キナーゼ阻害剤とその製造法
JPH08176070A (ja) 1994-12-19 1996-07-09 Mitsubishi Chem Corp ジデプシド誘導体及びｐｉ３キナーゼ阻害剤
JPH08336393A (ja) 1995-04-13 1996-12-24 Mitsubishi Chem Corp 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法
GB9521987D0 (en) 1995-10-26 1996-01-03 Ludwig Inst Cancer Res Phosphoinositide 3-kinase modulators
EP0876375A1 (en) 1995-11-17 1998-11-11 E.I. Du Pont De Nemours And Company Tricyclic herbicidal heterocycles
US6602677B1 (en) 1997-09-19 2003-08-05 Promega Corporation Thermostable luciferases and methods of production
DE19908538A1 (de) 1999-02-26 2000-08-31 Aventis Pharma Gmbh Polycyclische 2-Amino-Thiazol Systeme, Verfahren zu ihrer Herstellung und Arzneimittel enthaltend diese Verbindungen
DE19908533A1 (de) 1999-02-26 2000-08-31 Aventis Pharma Gmbh Polycyclische Thiazol-Systeme, Verfahren zu ihrer Herstellung und Arzneimittel enthaltend diese Verbindungen
DE19908537A1 (de) 1999-02-26 2000-08-31 Aventis Pharma Gmbh Verwendung von polycyclischen 2-Amino-Thiazol Systemen zur Herstellung von Medikamenten zur Prophylaxe oder Behandlung von Obesitas
DE19908535A1 (de) 1999-02-26 2000-08-31 Aventis Pharma Gmbh Verwendung von polycyclischen Thiazol-Systemen zur Herstellung von Medikamenten zur Prophylaxe oder Behandlung von Obesitas
US7273880B2 (en) 1999-06-30 2007-09-25 H. Lunbeck A/S Selective NPY (Y5) antagonists
ATE245636T1 (de) 1999-07-29 2003-08-15 Lilly Co Eli Benzofurylpiperazine: 5-ht2c serotoninrezeptor agonisten
JP2001247477A (ja) 2000-03-03 2001-09-11 Teikoku Hormone Mfg Co Ltd 抗腫瘍剤
WO2001064675A1 (en) * 2000-03-03 2001-09-07 Novartis Ag Condensed thiazolamines and their use as neuropeptide y5 antagonists
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
DE60203260T2 (de) 2001-01-16 2006-02-02 Glaxo Group Ltd., Greenford Pharmazeutische kombination, die ein 4-chinazolinamin und paclitaxel, carboplatin oder vinorelbin enthält, zur behandlung von krebs
WO2002098863A1 (fr) * 2001-06-05 2002-12-12 Fujisawa Pharmaceutical Co., Ltd. Derive d'imidazole fondu
EP1417976A4 (en) 2001-07-26 2004-09-15 Santen Pharmaceutical Co Ltd AGENT FOR TREATING GLAUKOM WITH A COMPOUND WITH PI3-KINASE INHIBITING EFFECT
US6703414B2 (en) 2001-09-14 2004-03-09 Arizona Board Of Regents On Behalf Of The University Of Arizona Device and method for treating restenosis
WO2003035618A2 (en) 2001-10-24 2003-05-01 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
WO2003034997A2 (en) 2001-10-24 2003-05-01 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
WO2003037886A2 (en) 2001-10-30 2003-05-08 Pharmacia Corporation Heteroaromatic carboxamide derivatives for the treatment of inflammation
EP1531813A1 (en) 2002-07-10 2005-05-25 Applied Research Systems ARS Holding N.V. Use of compounds for increasing spermatozoa motility
MXPA05000453A (es) 2002-07-10 2005-03-23 Applied Research Systems Derivados de benceno fusionados a azolidinona-vinilo.
US20040092561A1 (en) 2002-11-07 2004-05-13 Thomas Ruckle Azolidinone-vinyl fused -benzene derivatives
BR0312780A (pt) 2002-07-19 2005-05-03 Pharmacia Corp Compostos de tiofeno-carboxamida substituìda para o tratamento de inflamação
AU2003255845A1 (en) 2002-08-22 2004-03-11 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
WO2004069245A1 (en) * 2003-02-07 2004-08-19 Warner-Lambert Company Llc Oxazolidinone derivates n-substituted by a tricyclic ring, for use as antibacterial agents
EP1449844A1 (en) * 2003-02-14 2004-08-25 Ferring B.V. benzamide derivatives as oxytocin agonists and vasopressin antagonists
US20050239767A1 (en) 2003-10-28 2005-10-27 Chan Michael K Intermolecular SNAr of the heterocycle-activated nitro and fluoro groups-application in the synthesis of polyazamacrocyclic ligands
AU2005293607A1 (en) 2004-10-07 2006-04-20 Boehringer Ingelheim International Gmbh PI3 kinases
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
AU2006302415B2 (en) 2005-10-07 2012-09-13 Exelixis, Inc. Azetidines as MEK inhibitors for the treatment of proliferative diseases
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
DE602007007323D1 (de) 2006-04-26 2010-08-05 Hoffmann La Roche Thienoä3,2-düpyrimidin-derivat geeignet als pi3k inhibitor
MX2008013583A (es) 2006-04-26 2008-10-31 Genentech Inc Compuestos del inhibidor de fosfoinositido 3-cinasa y composiciones farmaceuticas que los contienen.
EP2054058B1 (en) 2006-08-04 2016-11-09 Beth Israel Deaconess Medical Center Inhibitors of pyruvate kinase and methods of treating disease
US7649007B2 (en) 2006-08-15 2010-01-19 Wyeth Llc Oxazolidine derivatives as PR modulators
US8779154B2 (en) * 2006-09-26 2014-07-15 Qinglin Che Fused ring compounds for inflammation and immune-related uses
EP2518074B1 (en) 2006-12-07 2015-07-22 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
ES2571028T3 (es) 2006-12-07 2016-05-23 Genentech Inc Compuestos inhibidores de fosfoinositida 3-cinasa y métodos de uso
CL2009000780A1 (es) * 2008-03-31 2010-01-15 Genentech Inc Compuestos derivados de heterociclil-pirano-heterociclilo, heterociclil-oxepina-heterociclilo, benzopirano-heterociclilo y benzoxepina-heterociclilo sustituidos; composicion farmaceutica; procedimiento de preparacion de la composicion; kit farmaceutico; y su uso en el tratamiento del cancer, mediado por la inhibicion de pi3k.
SI2483278T1 (sl) * 2009-09-28 2014-03-31 F. Hoffmann-La Roche Ag Inhibitorske spojine benzoksazepina pi3k in njihova uporaba pri zdravljenju raka
UA108863C2 (ru) * 2009-09-28 2015-06-25 Ф. Хоффманн-Ля Рош Аг Бензоксепиновые ингибиторы pi3 и их применение

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